With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.40283-41-8,2-Aminothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.
A solution of 2-amino-1,3-thiazole-4-carboxylic acid (85 mg, 0.59 mmol), TBTU (227 mg, 0.708 mmol), tert-butylpiperidin-4-ylcarbamate (236 mg, 1.18 mmol) and DIPEA (0.403 mL, 2.36 mmol) in dry DME (5 mL) was let understirring at rt overnight. The mixture was then diluted with EtOAc, washed with a saturated solution of NaHCO3, water and brine, dried over Na2SO4 and filtered. The title compound was purified by column chromatography (eluant DCM:MeOH = 98:2) and isolated as light yellow solid (147 mg, 77%).1H NMR (500 MHz, DMSO-d6) ppm 1.21 – 1.32 (m, 2 H) 1.38 (s, 9 H) 1.65- 1.81 (m, 2 H) 2.71 -2.90 (m, 1 H) 2.96- 3.15 (m, 1 H) 3.44 -3.57 (m, 1 H) 4.21 -4.32 (m, 2 H) 6.88 (d, J=7.93 Hz, 1 H) 6.92 (s, 1 H) 7.10 (s, 2 H).HRMS (ESI+): calcd. for C14H23N403S [M + H] 327.1486; found 327.1473., 40283-41-8
The synthetic route of 40283-41-8 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; CASALE, Elena; CORTI, Emliana; GNOCCHI, Paola; NESI, Marcella; ORRENIUS, Sten, Christian; QUARTIERI, Francesca; RICCARDI SIRTORI, Federico; (138 pag.)WO2018/19681; (2018); A1;,
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